Fezagepras sodium

CAS: 1254472-97-3 F: C13H17NaO2 W: 228.26

Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GP

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Bioactivity	Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84[1]. Fezagepras sodium decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2].
Target	GPR40, GPR84
Invitro	Fezagepras sodium (500 µM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].Fezagepras sodium (250 or 500 µM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis[2]. Cell Proliferation Assay[2] Cell Line:
In Vivo	Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS-/-db/db mice[1]. Animal Model:
Name	Fezagepras sodium
CAS	1254472-97-3
Formula	C13H17NaO2
Molar Mass	228.26
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Li Y, et al. Fatty acid receptor modulator PBI-4050 inhibits kidney fibrosis and improves glycemic control. JCI Insight. 2018 May 17;3(10). pii: 120365. [2]. Grouix B, et al. PBI-4050 Reduces Stellate Cell Activation and Liver Fibrosis through Modulation of Intracellular ATP Levels and the Liver Kinase B1/AMP-Activated Protein Kinase/Mammalian Target of Rapamycin Pathway. J Pharmacol Exp Ther. 2018 Oct;367(1):